CAS number：864070-44-0
molecular formula：C23H27ClO7
molecular weight：450.91
EINECS number：620-176-8

English synonyms

Empagliflozin(W.S);Empaglifloin;Empagliflozin API;BI-10773;BI 10773;BI10773;CS-798;EMPAGLIFLBZIN;EMpagliflozin;BI-10773

Related categories

Empagliflozin; raw materials and their intermediates; hypoglycemics; empagliflozin, API; API; hypoglycemic; small molecule inhibitors; pharmaceutical raw materials; small molecule inhibitors, natural products; Sugar drug; raw material drug [for scientific research only]; raw material drug; G protein coupled receptor & G protein; reference substance-impurity reference substance; chemical intermediate; anti-sugar; medical raw material; impurity reference substance; Products; pharmaceutical raw materials; raw materials; pharmaceutical raw materials; Empagliflozin intermediate series; API; Inhibitors; Empagliflozin; hormone regulation; fine chemical products; organic chemical raw materials; chemical raw materials; chemical reagents; chemical raw materials

Introduction

Empagliflozin, a type 2 sodium-glucose cotransporter (SGLT-2, sodium-dependentglucose cotransporter 2) inhibitor jointly developed by Boehringer Ingelheim and Eli Lilly and Company. SGLT-2 inhibitor is a new type of hypoglycemic drug, mainly by inhibiting the expression of SGLT-2, reducing the reabsorption of glucose by the kidneys, increasing the excretion of glucose in urine, thereby reducing plasma glucose levels, and its hypoglycemic effect does not depend on in β-cell function and insulin resistance.

●  Empagliflozin is used for the treatment of 2 diabetic adult patients who have failed to achieve adequate blood sugar control through diet and exercise, in order to improve blood sugar control. It should not be used to treat patients with type 1 diabetes, patients with elevated blood or urine ketones (diabetic ketoacidosis), patients with severe kidney impairment, end-stage kidney disease, and patients on dialysis.

●  Under physiological conditions, the kidneys filter and reabsorb glucose into the circulatory system to maintain blood sugar balance in the body, and glucose enters the blood through the renal tubule lumen, and must cooperate with glucose co-transporters. SGLT2 acts as a sodium glucose co-transporter for glucose A form of cotransporter that blocks glucose reabsorption by the proximal convoluted tubule, reduces renal glucose reabsorption, increases urinary glucose excretion, and reduces plasma glucose levels. And the hypoglycemic effect does not depend on β cell function and is not affected by insulin resistance.

●  Using 5-bromo-2-chlorobenzoic acid as raw material, the intermediate (S)-4-bromo-1-chloro-2-(4-tetrahydro : furan-3-yloxy-benzyl)benzene, the intermediate is condensed with 2,3,4,6-tetra-O-trimethylsilyl-D-glucopyranosic acid 1,5-lactone , etherification, demethylation to get empagliflozin, total yield 29.8%, purity 99.13%